2. GPCR/G Protein Neuronal Signaling
  3. Neurokinin Receptor
  4. NK3R-IN-2

NK3R-IN-2 是一种口服有效的 NK3R 抑制剂，对人 NK3R 的 IC50 为330.50 nM。NK3R-IN-2 可以穿过血脑屏障。NK3R-IN-2 在 CHO-K1 细胞中具有优异的 NK3R 结合亲和力 (IC50 = 87.31 nM)。NK3R-IN-2 能有效抑制黄体生成素 (LH) 的水平。NK3R-IN-2 可用于激素相关疾病的研究。

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NK3R-IN-2 Chemical Structure

NK3R-IN-2 Chemical Structure

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NK3R-IN-2 相关抗体

Top Publications Citing Use of Products

查看 Neurokinin Receptor 亚型特异性产品:

查看所有亚型
NK1R NK2R NK3R

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NK3R-IN-2 is an orally active NK3R inhibitor with an IC50 of 330.50 nM for human NK3R. NK3R-IN-2 can pass through the blood-brain barrier. NK3R-IN-2 has excellent NK3R binding affinity (IC50 = 87.31 nM) in CHO-K1 cells. NK3R-IN-2 effectively inhibits the level of luteinizing hormone (LH). NK3R-IN-2 can be used for research on hormone related conditions[1].

IC50 & Target

NK3R

 

体外研究
(In Vitro)

NK3R-IN-2 (Compoud 22i) (1 μM) 在人和大鼠肝微粒体中显示出良好的代谢稳定性[1]。
NK3R-IN-2 (0.3-30 μM) 对 hERG 通道没有明显的抑制作用 (IC50 = 31.7 μM)，也没有明显的心脏毒性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

NK3R-IN-2 相关抗体:
体内研究
(In Vivo)

NK3R-IN-2 (Compoud 22i) (5 mg/kg; 灌胃; 单剂量) 在雄性 Sprague-Dawley 大鼠中表现出优异的血脑屏障通透性和低肝毒性[1]。
NK3R-IN-2 (70 mg/kg; 灌胃; 单剂量) 显著抑制去卵巢 (OVX) Sprague-Dawley 大鼠的黄体生成素 (LH) 水平[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats (6-8 weeks, 180-220g)[1]
Dosage: 5 mg/kg
Administration: Oral gavage (i.g.); once at 1, 4 and 10 hours
Result: Was slightly higher than the level of ESN364 (HY-19632) in the brain.
Had a low concentration in the liver.
Animal Model: Ovariectomized (OVX) Sprague-Dawley rats (6-8 weeks, 180-220g)[1]
Dosage: 70 mg/kg
Administration: Oral gavage (i.g.); single dose
Result: Significantly reduced plasma LH concentration.
分子量

416.86

Formula

C18H14ClFN6OS
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

NK3R-IN-2 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NK3R-IN-2Neurokinin ReceptorNK receptorTachykinin receptorNK3RAntagonistEndocrinologyluteinizing hormoneInhibitorinhibitorinhibit

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目录号：
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